KR900012893A - 치환된-아세트 아미드 화합물 및 그 제조방법 - Google Patents

치환된-아세트 아미드 화합물 및 그 제조방법 Download PDF

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KR900012893A
KR900012893A KR1019900001846A KR900001846A KR900012893A KR 900012893 A KR900012893 A KR 900012893A KR 1019900001846 A KR1019900001846 A KR 1019900001846A KR 900001846 A KR900001846 A KR 900001846A KR 900012893 A KR900012893 A KR 900012893A
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alkyl
compound
hydroxy
formula
salt
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요우이치 시오카와
카즈오 오쿠무라
카즈히코 타케
카즈노리 츠바키
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후지사와 도모키치로
후지사와 야쿠힝 코교 가부시기가이샤
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Publication of KR900012893A publication Critical patent/KR900012893A/ko

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Abstract

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Description

치환된-아세트 아미드 화합물 및 그 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 일반식(Ⅰ)의 치환된-아세트아미드 화합물 및 그 약학적 허용염.
    상기식중, R1은 하나 이상의 적합한 치환체(들)을 가질 수 있는 아릴이고, R2는 하나이상의 적합한 치환체(들)을 가질 수 있는 아릴이거나, 저급알킬 또는 시클로(저급)알킬이고, R3는 수소, 히드록시, 할로겐, 저급 알케닐, 아미노 또는 보호된 아미노이고, R4는 식(여기에서, R5는 하나이상의 적합한 치환체(들)을 가질 수 있는 저급알킬기이거나, 시클로(저급)알킬,아릴, 또는 하나이상의 적합한 치환체(들)을 가질수 있는 아르(저급)알킬이고, R6은 수소 또는 저급알킬이다), 또는 하나이상의 적합한 치환체(들)을 가질 수 있는 N-함유 헤테로시클릭기이고, A는 저급알킬렌 또는 저급알키닐렌이고, R1과 R2는 수소원자를 통해 결합될 수 있다.
  2. 제1항에 있어서, R1은 할로겐, 저급알킬 및 저급알콕시로 구성되는 군으로부터 선택되는 1 내지 3개의 적합한 치환체(들)을 가질 수 있는 페닐이고, R2는 할로겐, 저급알킬 및 저급알콕시로 구성된 군으로부터 선택되는 1내지 3개의 적합한 치환체(들)을 가질 수 잇는 페닐 : 저급알킬 : 또는 시킬로(저급)알킬이고, R3는 수소, 히드록시, 할로겐, 저급알케닐, 아미노 또는 보호된 아미노이고, R4는 식(여기에서, R5는 히드록시 및 보호된 카르복시로 구성된 군으로부터 선택되는 1 내지 3개의 적합한 치환체(들)을 가질 수 있는 저급알킬 : 시클로(저급)알킬 : 페닐 : 또는 1 내지 3개의 저급 알콕시를 가질 수 있는 페닐(저급)알킬이고, R6는 수소 또는 저급알킬이다.), 또는 피리딜, 테트라히드로피리딜, 이미다졸리디닐, 피페리딜, 피페라지닐, 모르폴리닐 및 3-이자비시클로 〔3,2·2〕노난일로 구성된 군으로부터 선택된 N-함유 헤테로시클릭기이고, 그 각각은 저급 알킬, 히드록시, 히드록시(저급)알킬, 아미노보호기 또는 시아노이미노를 가질 수 있으며, A는 저급 알킬렌 또는 저급알키닐렌이고 R1과 R2는 산소원자를 통해 결합될 수 있는 화합물.
  3. 제2항에 있어서, R1은 할로겐, 저급알킬 및 저급알콕시로 구성되는 군으로부터 선택되는 하나의 적합한 치환체를 가질 수 있는 페닐이고, R2는 할로겐, 저급알킬 및 저급알콕시로 구성된 군으로부터 선택되는 하나의 적합한 치환체를 가질 수 있는 페닐, 또는 시클로(저급)알킬이고, R3는 히드록시 또는 할로겐이고, R4는 식(여기에서, R5는 저급알킬, 히드록시(저급)알킬 또는 저급알콕시 카르보닐(저급)알킬이고 R6는 수소 또는 저급알킬이다) : 피리딜 : 저급알킬 또는 페닐(저급)알킬을 가질 수 있는 테트라히드로피리딜 : 시아노이미노를 가질 수 있는 이마다졸리디닐 : 저급알킬, 히드록시 또는 히드록시(저급)알킬을 가질 수 잇는 피페리딜 : 저급알킬을 가질 수 있는 피페라지닐 : 모르폴리닐 : 또는 3-아자비시클로 〔3.2.2〕노난일이고 A는 저급알킬렌 또는 저급 알키닐레인 화합물.
  4. 제3항에 있어서 R1은 페닐이고, R2는 각각 페닐 또는 시클로(저급)알킬이고 R3는 히드록시이고 R3는 히드록시 또는 할로겐이고, R4는 식(여기에서, R5는 저급알킬이고 R6수소 또는 저급알킬이다), 또는 저급알킬을 가질 수 있는 1,2,3,6-테트라히드로피리딜이고는 저급알킬렌 또는 저급 알키닐렌인 화합물.
  5. 제4항에 있어서, R1과 R2는 각각 페닐이고 R3는 히드록시이고 R4는|(여기에서, R5는 저급알킬이고 A는 저급알키닐렌인 화합물.
  6. 제5항에 있어서, R4는 식(여기에서, R5는 에틸이고 R6는 수소 또는 메틸이다)이고 A는 2-부티닐렌인 화합물.
  7. 제6항에 있어서, N-(4-에틸아미노-2-부티닐)-2-히드록시-2,2-디페닐아세트아미드와 N-〔4-(N-메틸에틸아미노)-2-부티〕-2-히드록시-2,2-디페닐아세트 아미드로 구성된 화합물로부터 선택되는 화합물.
  8. 제7항에 있어서, N-(4-에틸아미노-2-부티닐)-2-히드록시-2,2-디페닐아세트아미드인 화합물.
  9. 제4항에 있어서, R1은 페닐이고 R2는 시클로(저급)알킬이고, R3는 히드록시이고, R4는 식(여기에서, R5와 R6는 각각 저급알킬이다.)이고 A는 저급알키닐렌인 화합물.
  10. 제9항에 있어서, N-(4-디메틸아미노-2-부티닐)-2-시클로펜틸-2-히드록시-2-페닐 아세트아미드와 N-(4-디메틸아미노-2-부티닐)-2-시클로헥실-2-히드록시-2-페닐아세트아미드로 구성된 화합물로부터 선택되는 화합물.
  11. 제4항에 있어서, R1는 페닐이고 R2는 시클로(저급)알킬이고, R3는 히드록시 또는 할로겐이고 R4는 저급알킬을 가질 수 있는 1,2,3,6-테트라하이드로피리딜이고 A는 저급 알킬렌인 화합물.
  12. 제11항에 있어서, N-(1,2,3,6-테트라히드로피리딘-4-일)메틸-2-시클로헥실-2-히드록시-2-페닐아세트아미드, N-(1-에틸-1,2,3,6-테트라히드로피리딘-4-일)메틸-2-시클로헥실-2-히드록시-2-페닐아세아미드, 및 N-(1-에틸-1,2,3,6-테트라히드로피리딘-4-일)메틸-2-클로로-2-시클로헥실-2-페닐아세트 아미드로 구성된 화합물로부터 선택되는 화합물.
  13. Ⅰ) 일반식(Ⅱ)의 화합물 또는 그 염을 일반식(Ⅲ) 또는 그 염과 반응시키거나 : Ⅱ) 일반식(Ⅳ)의 화합물이거나 카르복시기의 그 반응유도체 또는 그 염을 일반식(Ⅴ)의 화합물이거나 아미노기의 그 반응유도체 또는 그염을 반응시키거나 : Ⅲ) 일반식(Ⅰa)의 화합물 또는 그 염을 할로겐의 히드록시기로의 전환반응시켜서 일반식(Ⅰb)의 화합물 또는 그 염을 제조하거나 : Ⅳ) 일반식(Ⅵ)의 화합물 또는 그 염을 저급알킬화제와 반응시켜서 일반식(Ic)의 화합물 또는 그 염을 제조 하거나; Ⅴ)일반식 (Id)의 화합물 또는 그 염을 아미노보호기제거반응시킴으로써, 일반식(Ⅰe)의 화합물 또는 그 염을 제조하거나 : Ⅵ) 일반식(Ⅶ)의 화합물 또는 그 염을 일반식(Ⅴ)의 화합물 또는 그 염과 반응시켜서 일반식(Ⅰf)의 화합물 또는 그 염을 제조하거나 : Ⅶ) 일반식(Ⅰg)의 화합물 또는 그 염을 아미노보호기 제거반응 처리하여 일반식(Ⅰh)의 화합물 또는 그 염을 제조함으로써 일반식(Ⅰ)의 치환된-아세트아미드 화합물 또는 그 염을 제조하는 방법.
    상기식중, R1은 하나이상의 적합한 치환체(들)을 가질 수 있는 아릴이고, R2는 하나이상의 적합한 치환체(들)을 가질 수 잇는 아릴이거나, 저급알킬 또는 시클로(저급)알킬이고, R3는 수소, 히드록시, 할로겐, 저급알케닐, 아미노 또는 보호된 아미노이고, R4는 식(여기에서, R5는 하나이상의 적합한 치환체(들)을 가질 수 있는 저급알킬이거나, 시클로(저급)알킬, 아릴, 또는 하나이상의 적합한 치환체(들)을 가질 수 있는 아르(저급)알킬이고, R6은 수소 또는 저급알킬이다), 또는 하나이상의 적합한 치환체(들)을 가질 수 있는 N-함유헤테로시클릭기이고, A는 저급알킬렌 또는 저급 알키닐렌이고, R1과 R2는 산소원자를 통해 결합될 수 있고 X는 이탈기이고, Ra3은 할로겐이고, Rb3은 히드록시이고, Ra2는 저급알킬이고, R7은 아미노보호기이고, 식은 하나이상의 치환체(들)을 가질 수 있는 N-함유 헤테로시클릭기이고, R8은 하나이상의 할로겐을 가질 수 있는 저급알킬이고, Rc3는 보호된 아미노이고, Rd3은 아미노이다.
  14. 일반식(Ⅱ)의 화합물 또는 그 염.
    상기식중, R1은 하나이상의 적합한 치환체(들)을 가지 수 있는 아릴이고, R2는 하나이상의 적합한 치환체(들)을 가질 수 있는 아릴이거나, 저급알킬 또는 시클로(저급)알킬이고, R3는 수소, 히드록시, 할로겐, 저급알케닐, 아미노 또는 보호된 아미노이고, A는 저급알킬렌 또는 저급알키닐렌이고, X는 이탈기이고, R1과 R2는 산소원자를 통해 결합될 수 있다.
  15. 활성성분으로서 제1항의 화합물 또는 그 약학적 허용염을 약학적 허용담체와 혼합된 상태로 포함하는 약학 조성물.
  16. 배뇨장애의 치료에 사용되는 제1항의 화합물 또는 그 약학적 허용염.
  17. 제1항의 화합물 또는 그 약학적 허용염을 사람 또는 동물에게 투여하는 배뇨장애의 치료방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900001846A 1989-02-14 1990-02-14 치환된-아세트 아미드 화합물 및 그 제조방법 KR900012893A (ko)

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